Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1993-06-22
1995-06-20
Mars, Howard T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514175, 514176, 514178, 514181, 514182, 540 28, 540 41, 540 44, 540106, 540107, 540108, 552520, 552540, 552548, 552553, 552554, 552593, 552598, 552610, 552646, 552648, C07J 700, C07J 2100, C07J 4100, C07J 4300
Patent
active
054261023
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to compounds of the general formula I ##STR2## in which either Ia) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, or R.sup.12 and R.sup.13 together represent a second bond, or represents a hydrogen atom, or R.sup.12 and R.sup.13 together represent a second bond, hydrogen atoms, C.sub.1 -C.sub.10 -acyloxy group, CH.sub.2 Z wherein n is 0, 1, 2, 3, 4 or 5 and Z represents a hydrogen atom, a cyano group or the radical --OR.sup.5 in which R.sup.5 .dbd.H, C.sub.1 -C.sub.10 -alkyl or C.sub.1 -C.sub.10 -acyl; the grouping --(CH.sub.2).sub.m C.tbd.C--Y wherein m is 0, 1 or 2 and Y represents a hydrogen, fluorine, chlorine, bromine or iodine atom, or a C.sub.1 -C.sub.10 -hydroxyalkyl, C.sub.1 -C.sub.10 -alkoxyalkyl or C.sub.1 -C.sub.10 -acyloxyalkyl radical; or the grouping --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.k CH.sub.2 R.sup.6 wherein p is 0 or 1 and k is 0, 1 or 2 and R.sup.6 represents a hydrogen atom, a hydroxy group, a C.sub.1 -C.sub.4 -alkoxy radical or a C.sub.1 -C.sub.4 -acyloxy radical, the .beta.-configuration and .alpha.-configuration, formula ##STR3## wherein x=1 or 2, R.sup.4 represents a hydrogen atom; a cyano group; a chlorine, fluorine, bromine or iodine atom; a trialkylsily group; a trialkylstannyl group; a straight-chain or branched, saturated or unsaturated, C.sub.1 -C.sub.8 -alkyl, -acyl or alkoxyalkyl radical; an amino group ##STR4## in which R.sup.7 and R.sup.8, each independently of the other, represents a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group; a corresponding amine oxide ##STR5## or the grouping --OR.sup.9 or --S(O).sub.i R.sup.9 in which i=0, 1 or 2 and R.sup.9 represents a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or 2-dimethylaminoethyl group; or R.sup.4 represents a heteroaryl radical of formula I.alpha. ##STR6## in which A represents a nitrogen, oxygen or sulphur atom, --B--D--E-- represents the sequence of elements --C--C--C--, --N--C--C-- or --C--N--C-- and R.sup.10 represents a hydrogen atom; a cyano group; a chlorine, fluorine, bromine or iodine atom; a trialkylsilyl group; a trialkylstannyl group; a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 -alkyl, -acyl or alkoxyalkyl radical; an amino group ##STR7## in which R.sup.7 and R.sup.8, each independently of the other, represents a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group; a corresponding amine oxide ##STR8## or the grouping --OR.sup.9 or --S(O).sub.i R.sup.9 in which i=0, 1 or 2 and R.sup.9 represents a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or 2-dimethylaminoethyl group; or R.sup.4 represents a heteroaryl radical of formula I.beta. ##STR9## in which A represents a nitrogen atom and --B--D--E-- represents the sequence of elements --C--C--C--, --N--C--C--, --C--N--C-- or --C--C--N-- and R.sup.10 has the meaning already given, or R.sup.4 represents a phenyl radical of formula I.gamma. ##STR10## in which R.sup.10 has the meaning already given, and the pharmacologically tolerable addition salts thereof with acids, to processes for their preparation, to pharmaceutical compositions containing those compounds, to their use for the manufacture of medicaments, and to the novel intermediates required therefor.
The invention relates especially to compounds in which X represents an oxygen atom.
The alkoxy, acyloxy, alkyl, acyl and hydroxyalkyl groups contained in R.sup.2, R.sup.3, R.sup.5 and Y in the general formula I shall each have from 1 to 10 carbon atoms, and the alkoxyalkyl or acyloxyalkyl groups in Y shall each have from 2 to 10 carbon atoms. There may be mentioned as preferred alkoxy groups methoxy, ethoxy, propoxy and isopropoxy groups, and of the acyl(oxy) groups, formyl(oxy), acetyl(oxy) and propionyl(oxy) are of particular importance.
The alkyl groups are especially methyl, ethyl, propyl, isopropyl and tert.-butyl groups and, of the hydroxyalkyl groups, the corresponding radicals substituted at any position by
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Chwalisz Krzysztof
Cleve Arwed
Michna Horst
Neef Gunter
Ottow Eckhard
Kestler Kimberly J.
Mars Howard T.
Schering Aktiengesellschaft
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